U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 2251 - 2260 of 3524 results

Status:
US Previously Marketed
First approved in 1970

Class (Stereo):
CHEMICAL (ABSOLUTE)



Cephaloglycin, first oral cephalosporin, was introduced in 1965, but is no longer in common use. It is an orally absorbed derivative of cephalosporin C. Cephaloglycin binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis.
Status:
US Previously Marketed
Source:
C-Quens by Eli lilly
(1965)
Source URL:
First approved in 1965
Source:
C-Quens by Eli lilly
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Chlormadinone acetate (CMA) is a derivative of naturally secreted progesterone that shows high affinity and activity at the progesterone receptor. It has an anti-estrogenic effect and, in contrast to natural progesterone, shows moderate anti-androgenic properties. CMA acts by blocking androgen receptors in target organs and by reducing the activity of skin 5alpha-reductase. It suppresses gonadotropin secretion and thereby reduces ovarian and adrenal androgen production. CMA shows high contraceptive efficacy by inhibiting ovulation due to its ability to suppress or disrupt endogenous gonadotropin secretion and, by this, inhibits follicular growth and maturation. In addition, it suppresses endometrial thickness and increases the viscosity of cervical mucus. Chlormadinone acetate was withdrawn from the market in the USA, but it is still being used in Europe under the name Belara.
Status:
US Previously Marketed
First approved in 1964
Source:
Anavar by Searle
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Oxandrolone is a synthetic, orally active anabolic-androgenic steroid. Oxandrolones interact with androgen receptors in target tissues. Oxandrin is indicated as adjunctive therapy to promote weight gain after weight loss following extensive surgery, chronic infections, or severe trauma, and in some patients who without definite pathophysiologic reasons fail to gain or to maintain normal weight, to offset the protein catabolism associated with prolonged administration of corticosteroids, and for the relief of the bone pain frequently accompanying osteoporosis. Side effects include: elevated aminotransferases (ALT, AST), lipid abnormalities (e.g., decreased HDL cholesterol concentrations). Cardiovascular side effects have included edema, with and without congestive heart failure. Oxandrolone may inhibit the metabolism of oral hypoglycemic agents. In patients with edema, concomitant administration with adrenal cortical steroids or ACTH may increase the edema.
Status:
US Previously Marketed
Source:
RACOBALAMIN 57 DIAG by ABBOTT
(1963)
Source URL:
First approved in 1963
Source:
RACOBALAMIN 57 DIAG by ABBOTT
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Chlorprothixene (Taractan, Tarasan, Truxal) is a thioxanthine derivative developed by Lundbeck for the treatment of psychotic disorders. The drug exerts its activity by binding to and inhibiting serotonin receptors, dopamine receptors, muscarinic acetylcholine receptor, histamine H1 receptor and alpha1-adrenergic receptor.
Denatonium, usually available as denatonium benzoate (trade names Bitrex) is the most bitter chemical compound known, with bitterness thresholds of 0.05 ppm for the benzoate and 0.01 ppm for the saccharide. Scientists at Macfarlan Smith, Ltd. of Edinburgh, Scotland discovered Bitrex during research on derivatives of the anesthetic lidocaine. The extremely bitter taste proved effective in reducing ingestion by humans and animals. Denatonium is commonly included in placebo medications used in clinical trials to match the bitter taste of certain medications. Denatonium activates bitter taste receptor, mainly, TAS2R4, TAS2R8, TAS2R10, TAS2R13 on many cell types and plays important roles in chemical release, ciliary beating and smooth muscle relaxation through intracellular Ca(2+)-dependent pathways.
Status:
US Previously Marketed
Source:
Monase by Upjohn
(1961)
Source URL:
First approved in 1961
Source:
Monase by Upjohn
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Conditions:

ETRYPTAMINE (MONASE®), similar to the hallucinogenic tryptamines, is an inhibitor of monoamine oxidase, introduced for use as an antidepressant. It was withdrawn from the market due to problems with agranulocytosis and other side effects. However, it's activity is still under scientific investigation.
Status:
US Previously Marketed
First approved in 1961

Class (Stereo):
CHEMICAL (ABSOLUTE)



Paramethasone acetate (a derivative of paramethasone) is a glucocorticoid with the general properties of corticosteroids. It has been used by mouth in the treatment of all conditions in which corticosteroid therapy is indicated except adrenal-deficiency states for which its lack of sodium-retaining properties makes it less suitable than hydrocortisone with supplementary fludrocortisone.
Status:
US Previously Marketed
Source:
Diloderm by Schering
(1960)
Source URL:
First approved in 1960
Source:
Diloderm by Schering
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
US Previously Marketed
First approved in 1959
Source:
Laverna by Winthrop
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:


Oxyphenisatin is a stimulant laxative that has been used by mouth and as an enema. Oxyphenisatin was introduced as Lavema by Winthrop in US in 1959. Oxyphenisatin was used as a cleansing enema apart from x-ray studies and prior to urinary, gastro-intestinal and cholecystography x-ray examination. Oxyphenisatin was also used for preoperative preparation of the large intestine and colon. May be mixed with barium for x-ray examination of the large intestine. Oxyphenisatin may cause jaundice. Oxyphenisatin-induced liver damage usually occurs when the drug has been taken for at least six months and usually two years. Oxyphenisatin was withdrawn in most countries in the early 1970s.

Showing 2251 - 2260 of 3524 results